CGP-42112

CAS No. 127060-75-7

CGP-42112( CGP42112 | CGP 42112 | CGP-42112A )

Catalog No. M11134 CAS No. 127060-75-7

CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    CGP-42112
  • Note
    Research use only, not for human use.
  • Brief Description
    CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM.
  • Description
    CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM; significantly inhibits cGMP production from the basal value, also significantly inhibits TH-enzyme activity from the basal value in cultured porcine adrenal medullary cells; antagonizes Ang-II induced contractions in rabbit aortic rings with IC50 of 1.85 uM.
  • In Vitro
    CGP-42112 (≥1 nM) significantly inhibits cGMP production from the basal value. CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity from the basal value. These inhibitory effects of CGP-42112 on TH-enzyme activity and-cGMP production are abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) is ineffective. CGP-42112 binds selectively to the AT2 angiotensin II receptor subtype. [125I]CGP-42112 binds with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP-42112 binding in the brain, but does not alter its binding in the adrenal. CGP-42112 binds with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). CGP-42112 binding is selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 and the non-selective peptides Ang II and angiotensin III (Ang III).
  • In Vivo
    Intravenous infusions of CGP-42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF.
  • Synonyms
    CGP42112 | CGP 42112 | CGP-42112A
  • Pathway
    GPCR/G Protein
  • Target
    Angiotensin Receptor
  • Recptor
    Angiotensin Receptor
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    127060-75-7
  • Formula Weight
    1052.185
  • Molecular Formula
    C52H69N13O11
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 350 mg/mL
  • SMILES
    CC[C@H](C)[C@@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@H](CCCCNC([C@H](CCCNC(N)=N)NC(OCC3=CC=CC=C3)=O)=O)NC([C@H](CC4=CC=C(O)C=C4)NC(C5=CC=CN=C5)=O)=O)=O)=O)CCC1)=O
  • Chemical Name
    L-Isoleucine, N-(3-pyridinylcarbonyl)-L-tyrosyl-N6-[N2-[(phenylmethoxy)carbonyl]-L-arginyl]-L-lysyl-L-histidyl-L-prolyl-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hakam AC, et al. Am J Physiol Renal Physiol. 2006 Jun;290(6):F1430-6. 2. Takekoshi K, et al. Biochem Biophys Res Commun. 2000 Jun 7;272(2):544-50. 3. N?veri L, et al. J Cereb Blood Flow Metab. 1994 Jan;14(1):38-44. 4. N?veri L, et al. Acta Physiol Scand Suppl. 1995;630:1-48.
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